| 主权项 |
1. A peptide conjugate having the formula I
R1—Za-La-Ya—R2 (I) wherein R1 is H, C1-4 alkyl, acetyl, formyl, benzoyl or trifluoroacetyl; and R2 is OH or NH2; Za is a peptide sequence having the formula Ia
His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Z9-Leu-Ser-Z12-Z13-Z14-Glu-Z16-Glu-Ala-Val-Z20-Leu-Phe-Ile-Z24-Z25-Leu-Z27-Z28 (Ia) wherein Z9 is selected from Asp and Glu; Z12 is selected from Lys, Arg and Orn; Z13 is selected from Gln and Tyr; Z14 is selected from Met and Leu; Z16 is selected from Glu, Arg, Orn, Cys and Lys; Z20 is selected from Arg, Lys and Orn; Z24 is selected from Arg, Orn, Lys and Glu; Z25 is selected from Trp, Lys, Cys and Phe; Z27 is selected from Lys, Arg and Orn; and Z28 is selected from Asn and Asp or is absent; La is a peptide sequence having the formula Ib
L1-L2-L3-L4 (Ib) wherein L1 is selected from Orn, 8Ado, Cys, Lys and Gln or is absent; L2 is selected from Orn, 8Ado, Cys, Lys and Gln or is absent; L3 is selected from Orn, 8Ado, Cys, Lys and Gln or is absent; and L4 is selected from Orn, 8Ado, Cys, Lys and Gln or is absent; and at least one of L1, L2, L3 and L4 is 8Ado; Ya is a peptide sequence having the formula Ic
Y12-Y13-Y14-Y15-Asp-Y17 (Ic) wherein Y12 is selected from Tyr and Ala or is absent; Y13 is selected from Gly and Ala or is absent; Y14 is selected from Trp, 1Nal and Phe; Y15 is selected from Met, Leu, Nle, Thr and Phe; and Y17 is selected from Phe and 3-(3-pyridyl)-alanine; wherein at least one of Lys, Orn or Cys in formula Ia and Ib is further conjugated to a lipophilic and/or a biotinyl substituent and/or pegylated; or a pharmaceutically acceptable salt or solvate thereof. |
